1. Field of the Invention
This invention relates to a novel therapeutical agent for treating AIDS and related diseases, as well as to its preparation and use.
2. Field of the Invention
AIDS or acquired immunodeficiency syndrome is a pandemic disease characterized by a high susceptibility to unusual malignancies and immune impairment associated with life-threatening infections. The etiologic agent of AIDS has been identified as a retrovirus called HTLV-III/LAV or human T-cell lymphotropic virus type III/lymphadenopathy-associated virus. Throughout this specification, the retrovirus will be called HIV or human immunodeficiency virus as suggested in Science 232, 1486 (1986). Some other viruses related to HIV and causing diseases or conditions related to AIDS have recently been described.
It is known already that 3'-azido-2',2'-dideoxythymidine (azidothymidine, AZT), is a potent inhibitor of HIV replication in lymphocyte cultures and that it will protect the cells against the cytopathic effect of that virus at a concentration of 5 to 10 .mu.M (Mitsuya et al., Proc. Nat. Acad. Sci., USA, 82, 7096-7100 (1985). Further, it is known that 2',3'-dideoxyribosyl derivatives of purines (adenine, guanine, hypoxanthine) and pyrimidines (thymine and cytosine) significantly suppress the HIV-induced cytopathogenicity in vitro. The most potent derivative of the series is 2',3'-dideoxycytidine which will effect a complete antiviral protection at a concentration as low as 0.5-1.0 .mu.M (Mitsuya et al., Proc. Nat. Acad. Sci., USA, 83, 1911-1915 (1986).
In addition to this known matter, there is need for other substances acting as potential HIV-inhibitors and therefore, the invention has for its primary object to provide such inhibitors as well as therapeutic compositions containing the same.